The work proposed relates to the synthesis and pharmacological evaluation of new and optically pure antipsychotic (neuroleptic), antidepressant, antiparkinson, anticonvulsant, and antihistaminic drugs. While we are interested in preparing compounds of clinical significance we also plan to study basic pharmacological mechanisms of action and stereostructure-action relationships. Since all drugs proposed to be synthesized are prepared from amino acids of known absolute configuration the absolute configuration of the final drugs will also be known. Optical purity of intermediate and final compounds will be verified by ORD and/or CD analysis. Optically pure compounds will be evaluated by established methods for the above mentioned activities. Biological evaluation will include pharmacological testing in vivo and in vitro, behavioral and biochemical studies. In addition to our primary interest in studying drugs useful for treating diseases of the central nervous system (psychosis, depression, Parkinson's disease and epilepsy) we will examine some selected antagonists on the H2 histamine reseptor; i.e. histamine induced gastric acid secretion. Such antagonists have potential clinical significance in the therapeutic treatment of gastric ulcers.